Arformoterol tartrate Inhalation Solution is indicated for the long term, twice daily (morning and evening) maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. Itis for use by nebulization only.
selective long-acting beta2- adrenergic receptor agonist
Arformoterol, the (R,R)-enantiomer of formoterol, is a selective long-acting beta2
adrenergic receptor agonist (beta2-agonist) that has two-fold greater potency than racemic
formoterol (which contains both the (S,S) and (R,R)-enantiomers). The (S,S)-enantiomer is
about 1,000-fold less potent as a beta2-agonist than the (R,R)-enantiomer. While it is
recognized that beta2-receptors are the predominant adrenergic receptors in bronchial smooth
muscle and beta1-receptors are the predominant receptors in the heart, data indicate that there
are also beta2-receptors in the human heart comprising 10% to 50% of the total betaadrenergic receptors. The precise function of these receptors has not been established, but
they raise the possibility that even highly selective beta2-agonists may have cardiac effects.
The pharmacologic effects of beta2-adrenoceptor agonist drugs, including
arformoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the
enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′
adenosine monophosphate (cyclic AMP). Increased intracellular cyclic AMP levels cause
relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate
hypersensitivity from cells, especially from mast cells.
In vitro tests show that arformoterol is an inhibitor of the release of mast cell
mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also
inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and
inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The
relevance of these in vitro and animal findings to humans is unknown.
Other adrenergic drugs may potentiate effect. Xanthine derivatives, steroids, diuretics, or non-potassium sparing diuretics may potentiate hypokalemia or ECG changes. MAO inhibitors, tricyclic antidepressants and drugs that prolong the QTc interval may potentiate effect on the cardiovascular system. Beta-blockers may decrease effectiveness.
Asthenia, fever, bronchitis, COPD, headache, vomiting, hyperkalemia, leukocytosis, nervousness, and tremor.
Arformoterol has been shown to be teratogenic in rats based upon findings of omphalocele (umbilical hernia), a malformation, at oral doses of 1 mg/kg and above (AUC exposure approximately 370 times adult exposure at the maximum recommended daily inhalation dose). Increased pup loss at birth and during lactation and decreased pup weights were observed in rats at oral doses of 5 mg/kg and above (AUC exposure approximately 1100 times adult exposure at the maximum recommended daily inhalation dose). Delays in development were evident with an oral dose of 10 mg/kg (AUC exposure approximately 2400 times adult exposure at the maximum recommended daily inhalation dose).
Nursing Mothers In reproductive studies in rats, arformoterol was excreted in the milk. It is not known whether arformoterol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when it is administered to a nursing woman.
As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an overdose of Arformoterol nebuliser solution.
Arformoterol nebuliser solution should be stored at 2-8°C, protected from light and excessive heat. Do not freeze. Keep out of the reach of children.
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